Assay Detail
Functional
CHEMBL3107682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at P2Y1 receptor in washed human platelets assessed as 1 uM 2-methylthio-ADP-induced calcium flux by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.75 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3104624 | — | — | 1 | 8.66 |
| CHEMBL3104636 | — | — | 1 | 8.60 |
| CHEMBL3104625 | — | — | 1 | 8.23 |
| CHEMBL3105199 | — | — | 1 | 8.00 |
| CHEMBL3103635 | — | — | 1 | 7.98 |
| CHEMBL3105195 | — | — | 1 | 7.97 |
| CHEMBL2333770 | — | — | 1 | 7.54 |
| CHEMBL3105197 | — | — | 1 | 6.46 |
| CHEMBL3105198 | — | — | 1 | 6.30 |
| CHEMBL3105201 | — | — | 1 | - |
| CHEMBL3105200 | — | — | 1 | - |
| CHEMBL3105196 | — | — | 1 | - |
| CHEMBL3104626 | — | — | 1 | - |
| CHEMBL3103636 | — | — | 1 | - |
| CHEMBL3103634 | — | — | 1 | - |
| CHEMBL3103625 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3104624 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3104636 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3104625 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3105199 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3103635 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL3105195 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL2333770 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3105197 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL3105198 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL3105201 | — | IC50 | - | — | - | |
| CHEMBL3105200 | — | IC50 | - | — | - | |
| CHEMBL3105196 | — | IC50 | - | — | - | |
| CHEMBL3104626 | — | IC50 | - | — | - | |
| CHEMBL3103636 | — | IC50 | - | — | - | |
| CHEMBL3103634 | — | IC50 | - | — | - | |
| CHEMBL3103625 | — | IC50 | - | — | - |